Pharmaceutical Development and Technology最新文献

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Impact of critical process parameters on the dimensional, mean weight, and swelling properties of 3D-printed intravaginal rings: a quality by design approach. 关键工艺参数对3d打印阴道内环尺寸、平均重量和膨胀特性的影响:一种质量设计方法。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-02-01 Epub Date: 2025-02-14 DOI: 10.1080/10837450.2025.2462945
Gabrielle Silva de Campos Lazzarini, Guilherme Luíz Da Silva, Laís S Lacerda, Anna Lectícia M Martinez Toledo, Thaís Nogueira Barradas
{"title":"Impact of critical process parameters on the dimensional, mean weight, and swelling properties of 3D-printed intravaginal rings: a quality by design approach.","authors":"Gabrielle Silva de Campos Lazzarini, Guilherme Luíz Da Silva, Laís S Lacerda, Anna Lectícia M Martinez Toledo, Thaís Nogueira Barradas","doi":"10.1080/10837450.2025.2462945","DOIUrl":"10.1080/10837450.2025.2462945","url":null,"abstract":"<p><p>3D printing is emerging as a transformative technology in pharmaceutical manufacturing, enabling personalized medicine and innovative dosage forms. It allows precise control over drug release and dosage customization, addressing individual patient needs. Various 3D printing techniques, including fused deposition modeling (FDM), are being explored for pharmaceutical applications. The choice of polymers and their rheological properties is crucial for successful extrusion-based printing. While 3D printing accelerates drug development, challenges remain regarding quality control. Quality-by-design (QbD) approaches are essential to ensure safe and effective pharmaceutical products. This study highlights the role of critical process parameters (CPPs), such as infill density and printing speed, in producing poly(lactic acid)-based intravaginal rings. The effects of CPPs on critical quality attributes (CQAs), such as ring dimensions, weight, and swelling degree, were examined. Printing speed (25-100 mm/s) and infill density (0-20%) significantly affected weight and dimensions, with average weights ranging from 0.537 g to 0.629 g. Internal dimensions varied between 9.73 mm and 9.81 mm, while external dimensions ranged from 19.43 mm to 19.69 mm. Rings printed at the lowest speed and highest infill density showed the greatest swelling (2.47%). These findings confirm FDM as a viable method for producing cost-effective, patient-specific intravaginal rings with reproducible results.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"186-194"},"PeriodicalIF":2.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143123411","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation, characterisation and pharmacokinetics evaluation of dry power inhalation formulations of polymyxin B. 多粘菌素B干粉吸入制剂的制备、表征及药代动力学评价。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-02-01 Epub Date: 2025-02-14 DOI: 10.1080/10837450.2025.2462937
Yanna Yang, Yi Cheng, Jingyu Zhou, Jingnan Quan, Nan Liu, Zengming Wang, Hui Zhang, Xianggen Wu, Aiping Zheng
{"title":"Preparation, characterisation and pharmacokinetics evaluation of dry power inhalation formulations of polymyxin B.","authors":"Yanna Yang, Yi Cheng, Jingyu Zhou, Jingnan Quan, Nan Liu, Zengming Wang, Hui Zhang, Xianggen Wu, Aiping Zheng","doi":"10.1080/10837450.2025.2462937","DOIUrl":"10.1080/10837450.2025.2462937","url":null,"abstract":"<p><p>This study aims to develop an alternative and effective drug delivery system through inhalation therapy to address the limitations of polymyxin B (PMB) intravenous treatment for pneumonia. PMB dry powder inhalers (DPIs) were prepared and characterized. The in vitro lung deposition and antibacterial efficacy were also assessed. To compare the systemic exposure following changes in administration routes, blood concentration measurements were conducted for different routes of administration spherical PMB particles, measuring 3 microns in diameter, achieved the highest fine particle fraction (FPF) of 53%. When particles transition from regular shapes to irregular blocks, a decrease of 1 micron in particle size resulted in an approximate 20% increase in FPF. Moreover, the FPF of PMB particles combined with smooth-surfaced lactose was approximately 10% less than that of PMB particles combined with rough-surfaced mannitol. The bioavailability of PMB DPI reached a peak of 77.46% within 10 min. In a murine model of acute lung infection, treatment with PMB DPI significantly reduced the bacterial load in lung tissues compared to the control group with intravenous PMB administration. In summary, particles with reduced size and increased sphericity displayed a greater FPF led to enhanced therapeutic efficacy and safety.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"177-185"},"PeriodicalIF":2.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143190114","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Enhancing the efficacy of zinc oxide nanoparticles by beta-carotene conjugation for improved anti-microbial and anti-tumor therapy for dental application. 通过β -胡萝卜素偶联增强氧化锌纳米颗粒在牙科抗菌和抗肿瘤治疗中的作用。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-04 DOI: 10.1080/10837450.2024.2448620
Mohammed Rafi Shaik, Siva Prasad Panda, Shaik Althaf Hussain, Paramasivam Deepak, Nathiya Thiyagarajulu, Baji Shaik, Raghul Murugan, Ajay Guru
{"title":"Enhancing the efficacy of zinc oxide nanoparticles by beta-carotene conjugation for improved anti-microbial and anti-tumor therapy for dental application.","authors":"Mohammed Rafi Shaik, Siva Prasad Panda, Shaik Althaf Hussain, Paramasivam Deepak, Nathiya Thiyagarajulu, Baji Shaik, Raghul Murugan, Ajay Guru","doi":"10.1080/10837450.2024.2448620","DOIUrl":"10.1080/10837450.2024.2448620","url":null,"abstract":"<p><p>Zinc oxide NPs (ZnO NPs) are notable in nanomedicine for their exceptional physicochemical and biological properties. This study synthesizes and characterizes beta-carotene-coated ZnO NPs (BT-ZnO NPs) for potential anti-cancer and antimicrobial applications, demonstrating significant efficacy against dental pathogens and oral cancer cells. Scanning Electron Microscopy, EDAX, UV, FTIR, XRD, and Zeta potential analysis of prepared BT-ZnO NPs revealed uniform flower-like crystalline structures with intricate morphology and an average particle size of 38.06 nm. FTIR spectra identified various functional groups, suggesting a complex organic compound coated with ZnO NPs. Zeta potential measurements showed pH-dependent surface charge variations, which are crucial for understanding colloidal stability. The antimicrobial activity was potent against dental pathogens, with minimum inhibitory concentration (MIC) values of 50 µg/mL highlighting significant inhibition. Molecular docking studies demonstrated strong binding affinities of BT to key receptor proteins of dental pathogens. BT-ZnO NPs exhibited notable antioxidant activity of 68%, comparable to ascorbic acid, and significant anti-inflammatory effects of 75.1% at 100 µg/mL. Cytotoxicity assays indicated a concentration-dependent suppression of KB cell proliferation, decreasing cell viability to 37.19%, and gene expression studies showed elevated P53 expression, suggesting a strong apoptotic response. These multifaceted properties underscore the potential of BT-ZnO NPs as an integrated therapeutic approach for dental healthcare and oncology.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"101-113"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142907514","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
'Applications of machine learning in liposomal formulation and development'. 机器学习在脂质体配方和开发中的应用
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-11 DOI: 10.1080/10837450.2024.2448777
Sina Matalqah, Zainab Lafi, Qasim Mhaidat, Nisreen Asha, Sara Yousef Asha
{"title":"'Applications of machine learning in liposomal formulation and development'.","authors":"Sina Matalqah, Zainab Lafi, Qasim Mhaidat, Nisreen Asha, Sara Yousef Asha","doi":"10.1080/10837450.2024.2448777","DOIUrl":"10.1080/10837450.2024.2448777","url":null,"abstract":"<p><p>Machine learning (ML) has emerged as a transformative tool in drug delivery, particularly in the design and optimization of liposomal formulations. This review focuses on the intersection of ML and liposomal technology, highlighting how advanced algorithms are accelerating formulation processes, predicting key parameters, and enabling personalized therapies. ML-driven approaches are restructuring formulation development by optimizing liposome size, stability, and encapsulation efficiency while refining drug release profiles. Additionally, the integration of ML enhances therapeutic outcomes by enabling precision-targeted delivery and minimizing side effects. This review presents current breakthroughs, challenges, and future opportunities in applying ML to liposomal systems, aiming to improve therapeutic efficacy and patient outcomes in various disease treatments.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"126-136"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142952902","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Targeted delivery strategy of indocyanine green-mitoxantrone loaded liposomes co-modified with BTP-7 and BR2 for the treatment of glioma. BTP-7和BR2共修饰吲哚菁绿-米托蒽醌脂质体治疗胶质瘤的靶向递送策略
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-08 DOI: 10.1080/10837450.2024.2448619
Lin Jing, Jingguo Du, Yichao Dong, Lili Li, Zijun Tang, Xu Liu, Yonglong Zhong, Mingqing Yuan
{"title":"Targeted delivery strategy of indocyanine green-mitoxantrone loaded liposomes co-modified with BTP-7 and BR2 for the treatment of glioma.","authors":"Lin Jing, Jingguo Du, Yichao Dong, Lili Li, Zijun Tang, Xu Liu, Yonglong Zhong, Mingqing Yuan","doi":"10.1080/10837450.2024.2448619","DOIUrl":"10.1080/10837450.2024.2448619","url":null,"abstract":"<p><strong>Objective: </strong>This study aims to develop a dual-ligand-modified targeted drug delivery system by integrating photosensitizers and chemotherapeutic drugs to enhance anti-glioma effects. The system is designed to overcome the blood-brain barrier (BBB) that hinders effective drug delivery, increase drug accumulation in glioma cells, and thereby enhance therapeutic efficacy.</p><p><strong>Methods: </strong>Liposomes were prepared using the film dispersion-ammonium sulfate gradient technique, co-loading the photosensitizer indocyanine green (ICG) and the chemotherapeutic drug mitoxantrone (MTO). The conjugation of BTP-7 and BR2 to the liposome surface was achieved using an organic phase reaction method. The stability, dispersibility, particle size, and potential of the modified liposomes were tested. Their ability to penetrate the BBB and accumulate in glioma was evaluated in BBB models and cellular uptake studies. Additionally, the anti-tumor activity of this combination approach was assessed.</p><p><strong>Results: </strong>The resulting liposomes demonstrated significant stability and dispersibility, with an average particle size of 142.3 ± 1.8 nm and a potential of -17.6 mV. BBB model and cellular uptake studies indicated that BTP-7/BR2-ICG/MTO-LP could not only penetrate the BBB but also accumulate in glioma, leading to glioma cell necrosis. The anti-tumor activity evaluation showed that this combination approach exhibited a strong tumor-suppressing effect.</p><p><strong>Conclusion: </strong>The dual-ligand-modified liposomes developed in this study can penetrate the blood-brain barrier and achieve targeted drug delivery in glioma therapy. The combination of BTP-7 and BR2 not only enhances the carrier's penetration ability but also increases intracellular drug accumulation, thereby improving therapeutic efficacy. This novel therapeutic approach, which combines chemotherapy and photothermal response <i>via</i> dual-ligand-modified liposomes delivered to the tumor site, demonstrates the potential to reduce drug-related side effects and improve treatment outcomes.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"90-100"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142915393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Intensification of quercetin nanobubble formulation and performance by multi-factor optimization and interaction analysis. 多因素优化及交互作用分析强化槲皮素纳米泡配方及性能。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2024-12-31 DOI: 10.1080/10837450.2024.2441182
Hema Kumar A V, Chamakuri Kantlam
{"title":"Intensification of quercetin nanobubble formulation and performance by multi-factor optimization and interaction analysis.","authors":"Hema Kumar A V, Chamakuri Kantlam","doi":"10.1080/10837450.2024.2441182","DOIUrl":"10.1080/10837450.2024.2441182","url":null,"abstract":"<p><p>The natural flavonoid Quercetin (QT) showed a potential for various health benefits, but its pharmaceutical applications are hindered by low solubility, permeability, and limited bioavailability. This research aimed to synthesize, develop and optimize polylactic acid co-glycolic acid (PLGA) nanobubbles using solvent evaporation method as a sustained delivery system for QT, thus improving stability and bioavailability. Through a four-factor, three-level Box Behnken Design, 29 experimental runs were carried out to optimize QT-PLGA nanobubbles. An optimized formulation consisted of 50 mg QT, 250 mg PLGA, and 1.89% <i>w/v</i> PVA. The nanobubbles displayed a particle size of 139.5 ± 6.24 nm, polydispersity index of 0.296 ± 0.19, and zeta potential of -23.0 ± 3.44 mV, with an entrapment efficiency of 59.24 ± 3.08%. Analysis through Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction confirmed no drug-polymer interaction, while scanning electron microscopy revealed a uniform spherical nanoparticle. <i>In vitro</i> studies exhibited an excellent drug release, and stability studies showed no significant changes after one month. <i>In vivo</i> studies in rats demonstrated increased <i>C</i><sub>max</sub> (3.03) and <i>AUC</i><sub>0-t</sub> (5.84), indicating an improved sustained release and absorption. These findings underscored a potential of QT-loaded PLGA nanobubbles to enhance the drug kinetics and bioavailability, offering possibilities for targeted drug delivery and improved therapeutic outcomes.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"10-24"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142882569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Inhibition of growth and lung metastasis of breast cancer by pH-responsive methotrexate/curcumin-loaded chitosan-stabilized nanoemulsions. ph响应性甲氨蝶呤/姜黄素负载壳聚糖稳定纳米乳对乳腺癌生长和肺转移的抑制作用。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-10 DOI: 10.1080/10837450.2024.2448335
Mehrnoosh Nikpour, Zahra Karami, Samaneh Rafieenia, Arghavan Adibifar, Shaghayegh Yazdani, Fatemeh Saghatchi Zanjani, Tohid Mortezazadeh, Zahra Abdi, Kobra Rostamizadeh
{"title":"Inhibition of growth and lung metastasis of breast cancer by pH-responsive methotrexate/curcumin-loaded chitosan-stabilized nanoemulsions.","authors":"Mehrnoosh Nikpour, Zahra Karami, Samaneh Rafieenia, Arghavan Adibifar, Shaghayegh Yazdani, Fatemeh Saghatchi Zanjani, Tohid Mortezazadeh, Zahra Abdi, Kobra Rostamizadeh","doi":"10.1080/10837450.2024.2448335","DOIUrl":"10.1080/10837450.2024.2448335","url":null,"abstract":"<p><p>Chemotherapeutic agents are widely used to combat breast cancer. However, due to their non-selective biodistribution, their usage is associated with severe adverse effects on healthy tissues. In this study, a chitosan-stabilized nanoemulsion (CSNE) was prepared for the codelivery of curcumin (CUR) and methotrexate (MTX). The mean diameter and polydispersity index of CUR-MTX-CSNEs were 194.63 ± 6.7 nm and 0.27 ± 0.06, respectively. Modifying the nanoemulsion surface with chitosan decreased the drug release at pH 7.4 compared to pH 5.8. The MTT test demonstrated that CUR-MTX-CSNEs were more successful in reducing the cell viability of 4T1 cells than both bare formulation and free drugs. Moreover, compared to the free drug-treated group, a 2.6 times reduction of the relative tumor volume was witnessed in CUR-MTX-CSNEs-receiving mice. Histopathological studies confirmed a more substantial inhibitory effect on tumor growth and pulmonary metastasis of developed nanostructures than free CUR/MTX. While there was no noticeable toxicity in the vital organs of CUR-MTX-CSNEs-receiving mice, free drugs resulted in severe toxicity in the liver, kidney, lung and spleen. Overall, the pH-dependent drug release, improved anti-tumor activity and reduced organ toxicity suggest that CUR-MTX-CSNE may be promising in breast cancer therapy.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"57-68"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142952933","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formation and stabilization mechanism of Ginsenoside Rg3 inclusion complexes based on molecular simulation. 基于分子模拟的人参皂苷 Rg3 包合物的形成和稳定机制。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-11 DOI: 10.1080/10837450.2024.2448618
Shili Pan, Wei Shen, Xuehui Ding, Jingying Li, Jiahui Xu, Jixin Li, Ye Qiu, Wei Xu
{"title":"Formation and stabilization mechanism of Ginsenoside Rg3 inclusion complexes based on molecular simulation.","authors":"Shili Pan, Wei Shen, Xuehui Ding, Jingying Li, Jiahui Xu, Jixin Li, Ye Qiu, Wei Xu","doi":"10.1080/10837450.2024.2448618","DOIUrl":"10.1080/10837450.2024.2448618","url":null,"abstract":"<p><p>The formation of inclusion complexes between Ginsenoside Rg3 and cyclodextrins represents a promising strategy to enhance the solubility of G-Rg3. Nevertheless, the molecular mechanisms underlying the interaction between G-Rg3 and cyclodextrins have yet to be fully elucidated. In this study, we employed a combination of molecular simulation and experimental methodologies to identify the most effective solubilizing carriers among G-Rg3, β-cyclodextrin (β-CD), 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), and 2,6-dimethyl-β-cyclodextrin (DM-β-CD). The inclusion complexes formed with HP-β-CD demonstrates superior stability and water solubility compared to those formed with β-CD and DM-β-CD. The preparation process for the inclusion complexes of G-Rg3 and HP-β-CD was optimized through an orthogonal testing approach. The optimal conditions were determined to be a mass ratio of G-Rg3 to HP-β-CD of 1:125, an inclusion time of 2 h, and an inclusion temperature of 30 °C. The formation of the inclusion complexes was confirmed using DSC, Fourier Transform Infrared FTIR, and XRD techniques. <i>In vitro</i> solubility tests indicated that the solubility of the G-Rg3 inclusion complexes was 2.9 times greater than that of G-Rg3. Molecular dynamics (MD) simulations provided insights into the mechanisms that stabilize the inclusion complexes and enhance their water solubility. The primary interaction force between G-Rg3 and HP-β-CD was identified as the van der Waals force.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"79-89"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142915389","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Drug-silica-cellulose ternary matrix for the oral delivery of Cyclosporine A: in vitro and in vivo evaluation. 口服环孢素A的药物-硅-纤维素三元基质:体外和体内评价。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2025-01-19 DOI: 10.1080/10837450.2024.2448625
Pinal Chaudhari, Vivek M Ghate, Arun K Kodoth, Sumit Birangal, Shaila A Lewis
{"title":"Drug-silica-cellulose ternary matrix for the oral delivery of Cyclosporine A: <i>in vitro</i> and <i>in vivo</i> evaluation.","authors":"Pinal Chaudhari, Vivek M Ghate, Arun K Kodoth, Sumit Birangal, Shaila A Lewis","doi":"10.1080/10837450.2024.2448625","DOIUrl":"10.1080/10837450.2024.2448625","url":null,"abstract":"<p><strong>Purpose: </strong>Supersaturated formulations have been widely explored for improving the oral bioavailability of drugs by using mesoporous silica (MS) to generate supersaturation <i>via</i> molecular adsorption; however, this is followed by precipitation. Several precipitation inhibitors (PI) have been explored to prevent precipitation and maintain the drug in solution for a longer period. However, the combined approach of MS and PIs, the impact of MS and Silica, and the loading of high-molecular-weight neutral molecules such as Cyclosporine A (CsA) have not yet been explored. The present study aimed to explore the impact of MS and a hydroxypropyl methylcellulose (HPMC) matrix on the supersaturation and bioavailability of the neutral drug CsA.</p><p><strong>Methods: </strong>A CsA-loaded mesoporous silica/HPMC ternary matrix and CsA-HPMC and CsA-MS controls were prepared, and physicochemical characterization was carried out. The ternary matrix and controls were investigated for the Non-sink Mini FaSSIF dissolution and biorelevant transfer studies. Furthermore, drug release modeling was performed using DDSolver, and pharmacokinetic studies were performed to assess the impact on oral bioavailability compared with the marketed formulation.</p><p><strong>Results: </strong>The study suggested that the co-loaded CsA, HPMC, and MS demonstrated higher supersaturation than CsA-loaded silica and CsA-HPMC controls. A significant improvement in FaSSIF single medium (2-fold) and biorelevant transfer (3.37-fold) increase in the dissolution profile was observed for the co-loaded CsA-MS-HPMC samples. The <i>in vitro</i> dissolution profile was corroborated by pharmacokinetic studies, which showed a 1.19-fold higher oral bioavailability of CsA-MS-HPMC compared to that of CsA-MS and CsA-HPMC.</p><p><strong>Conclusion: </strong>The pharmacokinetics indicated that CsA-MS-HPMC co-loaded samples demonstrated supersaturation and improved bioavailability compared with the physical mixture.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"114-125"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142927378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Thermoresponsive biomaterial system of irinotecan and curcumin for the treatment of colorectal cancer: in-vitro and in-vivo investigations. 伊立替康和姜黄素的热响应性生物材料系统治疗结直肠癌:体内和体外研究。
IF 2.6 4区 医学
Pharmaceutical Development and Technology Pub Date : 2025-01-01 Epub Date: 2024-12-31 DOI: 10.1080/10837450.2024.2448334
Aleena Maryiam, Sibgha Batool, Zakir Ali, Fatima Zahid, Ali H Alamri, Taha Alqahtani, Adel Al Fatease, Ahmed A Lahiq, Muhammad Waseem Khan, Fakhar Ud Din
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